What is the use of Tolterodine (Detrol)?

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Last updated: May 23, 2025View editorial policy

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From the Guidelines

Tolterodine should be offered as a second-line therapy for the treatment of overactive bladder, as it has been shown to reduce symptoms, although it is commonly associated with non-life-threatening side effects, as stated in the 2012 AUA/SUFU guideline 1.

Key Points to Consider

  • The standard dosage for adults is typically 2 mg twice daily for immediate-release tablets or 4 mg once daily for extended-release capsules.
  • Lower doses (1 mg twice daily or 2 mg extended-release) may be recommended for patients with liver impairment or those taking certain medications that interact with tolterodine.
  • Common side effects include dry mouth, constipation, headache, and blurred vision.
  • Patients should take tolterodine with water and can take it with or without food.
  • The medication may take 1-2 weeks to show full effectiveness, so patients should continue taking it as prescribed even if improvement isn't immediate.

Important Considerations

  • Tolterodine should be avoided in patients with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, or myasthenia gravis.
  • It's essential to stay hydrated while taking this medication, but patients should avoid alcohol as it may worsen side effects like drowsiness and dizziness.
  • According to a 2023 European Association of Urology guideline, tolterodine has been shown to be effective in men with overactive bladder symptoms and presumed non-obstructive benign prostatic hyperplasia 1.

Side Effects and Interactions

  • Patients with more severe symptoms may experience greater symptom reductions, but those with relatively low baseline symptom levels are likely to experience complete symptom relief 1.
  • Tolterodine may interact with certain medications, such as anticholinergics, and may worsen side effects like dry mouth, constipation, and blurred vision.

From the FDA Drug Label

The FDA drug label does not answer the question.

From the Research

Tolterodine Overview

  • Tolterodine is a competitive muscarinic receptor antagonist that shows in vivo selectivity for the bladder over the salivary glands compared with oxybutinin 2.
  • It is used in the treatment of overactive bladder, with symptoms of urgency, frequency, and urge incontinence.

Efficacy

  • Tolterodine has been found to significantly reduce micturition frequency, urgency perception, and the number of episodes of urge incontinence, and increase the volume voided per micturition 3.
  • It is as effective as oxybutynin in improving micturition diary variables, but is associated with a significantly lower incidence and intensity of dry mouth 2, 4.
  • Tolterodine has been shown to maintain its clinical efficacy during long-term treatment, with significant improvements in micturitions per 24 hours, urge incontinence episodes per 24 hours, and volume voided per micturition after 9 months of treatment 5.

Tolerability

  • Dry mouth is the most frequently reported adverse event, but is mostly mild to moderate in severity 2, 5.
  • The incidence of dry mouth is lower with tolterodine than with oxybutynin, with a 23% lower incidence of dry mouth reported with once daily extended-release tolterodine capsules than with twice daily immediate-release tablets 2.
  • Tolterodine is well tolerated in elderly patients, with no serious tolerability concerns identified 2, 3.
  • The safety profile of tolterodine is similar in patients aged 65 years or older and in younger adults 3.

Comparison to Oxybutynin

  • Tolterodine is as effective as oxybutynin in improving urinary symptoms, but has superior tolerability 4.
  • Patients treated with tolterodine have significantly fewer adverse events, notably dry mouth, and a lower incidence of dose reduction than those in the oxybutynin group 4.
  • The adverse effect profiles of tolterodine and oxybutynin are similar, but comparative clinical trials have shown significantly fewer patients taking tolterodine require dosage reductions or discontinue therapy due to antimuscarinic adverse effects such as dry mouth 6.

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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